Synthesis and in vitro antitumor activity of novel scopoletin derivatives

被引：59

作者：

Liu, Wukun ^{[1
,2
]}

Hua, Jie ^{[3
]}

Zhou, Jinpei ^{[1
]}

Zhang, Huibin ^{[1
]}

Zhu, Haiyang ^{[1
]}

Cheng, Yanhua ^{[1
]}

Gust, Ronald ^{[4
]}

机构：

[1] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China

[2] Free Univ Berlin, Inst Pharm, D-14195 Berlin, Germany

[3] Jiangsu Jumpcan Pharmaceut Co Ltd, R&D Inst, Taixin 225441, Peoples R China

[4] Univ Innsbruck, Inst Pharm, A-6020 Innsbruck, Austria

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 15期

关键词：

Scopoletin; Scopoletin derivatives; Synthesis; Antitumor activity; NATURAL-PRODUCTS; DRUG DISCOVERY; CELL-LINE; INFLAMMATORY CYTOKINES; KAPPA-B; INHIBITION; COUMARIN; CANCER; APOPTOSIS; TARGET;

D O I：

10.1016/j.bmcl.2012.06.014

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Twenty scopoletin derivatives were developed by a systematic combinatorial chemical approach and their chemical structures were confirmed by MS, IR, H-1 NMR spectra and elemental analysis. Primary screening against mammary (MCF-7 and MDA-MB 231) and colon (HT-29) carcinoma cells indicated that five compounds (8d, 8g, 8j, 11b and 11g) displayed high antitumor potencies with IC50 values below 20 mu M whereas scopoletin showed IC50 values above 100 mu M. Moreover, the most promising compound 11g was more active than 5-fluorouracil. These results clearly indicated that the modification of the scopoletin structure could greatly increase its antitumor activity in vitro. (c) 2012 Elsevier Ltd. All rights reserved.

引用

页码：5008 / 5012

页数：5

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